Bis(acridinylthiourea)platinum(II) Complexes: Synthesis, DNA affinity, and biological activity in ghoblastoma cells

被引：25

作者：

Augustus, TM

Anderson, J

Hess, SM

Bierbach, U ^{[1
]}

机构：

[1] Wake Forest Univ, Dept Chem, Winston Salem, NC 27109 USA

[2] Wake Forest Univ, Sch Med, Dept Radiat Oncol, Winston Salem, NC 27157 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(02)01078-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The preparation of two novel bis(acridine)platinum(II) complexes is reported. The 4+ charged conjugates associate strongly with double-stranded native DNA (K-i > 10(6)), possibly through bisintercalation. A cell viability assay was used to demonstrate that both compounds are capable of mediating cytotoxicity at micromolar concentrations in SNB19 brain tumor cells. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

收藏

页码：855 / 858

页数：4

相关论文

共 18 条

[1] Mechanism of action of non-cisplatin type DNA-targeted platinum anticancer agents: DNA interactions of novel acridinylthioureas and their platinum conjugates [J].

Baruah, H ;

Rector, CL ;

Monnier, SM ;

Bierbach, U .

BIOCHEMICAL PHARMACOLOGY, 2002, 64 (02) :191-200

[2]

BARUAH H, 2002, MET MED GORD RES C N

[3] Modification of platinum(II) antitumor complexes with sulfur ligands.: 2.: Reactivity and nucleotide binding properties of cationic complexes of the types [PtCl(diamine)(L)]NO3 and [{PtCl(diamine)}2(L-L)](NO3)2 (L = monofunctional thiourea derivative; L-L = bifunctional thiourea derivative) in relation to their cytotoxicity [J].

Bierbach, U ;

Roberts, JD ;

Farrell, N .

INORGANIC CHEMISTRY, 1998, 37 (04) :717-723

[4] REACTIVITY OF GLUTATHIONE AND CYSTEINE TOWARD PLATINUM(II) IN THE PRESENCE AND ABSENCE OF GUANOSINE 5'-MONOPHOSPHATE [J].

BOSE, RN ;

MOGHADDAS, S ;

WEAVER, EL ;

COX, EH .

INORGANIC CHEMISTRY, 1995, 34 (23) :5878-5883

[5] Intercalators as anticancer drugs [J].

Braña, MF ;

Cacho, M ;

Gradillas, A ;

de Pascual-Teresa, B ;

Ramos, A .

CURRENT PHARMACEUTICAL DESIGN, 2001, 7 (17) :1745-1780

[6] Cytotoxic acridinylthiourea and its platinum conjugate produce enzyme-mediated DNA strand breaks [J].

Brow, JM ;

Pleatman, CR ;

Bierbach, U .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (20) :2953-2955

[7]

CROTEAU D, 2002, CURR TREAT OPTIONS O, V2, P507

[8]

Groothuis DR, 2000, NEURO-ONCOLOGY, V2, P45, DOI 10.1093/neuonc/2.1.45

[9]

Jenkins T C, 1997, Methods Mol Biol, V90, P195

[10] Design, synthesis, and biological activity of a novel non-cisplatin-type platinum-acridine pharmacophore [J].

Martins, ET ;

Baruah, H ;

Kramarczyk, J ;

Saluta, G ;

Day, CS ;

Kucera, GL ;

Bierbach, U .

JOURNAL OF MEDICINAL CHEMISTRY, 2001, 44 (25) :4492-4496